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During the course of our research on mGlu
2020-04-07

During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology,
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As a transcription factor HOXA regulates multiple target gen
2020-04-07

As a transcription factor, HOXA9 regulates multiple target genes related to cell growth, including BRCA1 [34], BCL-2 [35], c-MYB [36], IGF1 [37], PIM1 [38] and so on. In addition, HOXA9 is a member of both activating and repressive transcriptional regulatory complexes, along with cofactor and collab
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br Results br Discussion In this study we investigated the
2020-04-07

Results Discussion In this study, we investigated the role of EP4 on invasion and invadopodia in breast cancer cells. Our results demonstrate that EP4 activation promotes invadopodia-driven ECM degradation, in turn facilitating future intravasation and metastasis of breast cancer Quercetin dih
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br Acknowledgment We thank Professor Yuh Chang Sun for provi
2020-04-07

Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, achi
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Recently experimentally exposed common carp took up
2020-04-07

Recently, experimentally-exposed common carp took up CLO from water and maintained a consistent concentration in the liver and blood plasma (Corcoran et al., 2014). Clotrimazole may influence other aquatic organisms. Survival and development of marine shrimp larvae (Palaemon serratus) were affected
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The development of novel approaches to
2020-04-07

The development of novel approaches to study GPCR-mediated transactivation in live GSK-923295 receptor is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitm
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br Oxysterols as Key Players in
2020-04-07

Oxysterols as Key Players in Metabolic Syndrome? Obesity and sedentary lifestyle are on the rise and pose serious threats to people\'s health and wellbeing. Obesity is often associated with other pathologies and is one of the criteria included in the definition of metabolic syndrome (MetS) (see G
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PBMC derived macrophages not only express
2020-04-07

PBMC-derived macrophages not only express EBI2 but also have the ability to respond to their natural agonist 7α,25-OHC by activating downstream signal transduction pathways. In line with previous findings, our data confirm that receptor stimulation induces calcium mobilization which can be blocked b
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Despite the fact that the precise
2020-04-07

Despite the fact that the precise relevance of Ube2E self-ubiquitination in vivo is still elusive, findings of Sarkari et al. do establish Ube2E1 ubiquitination in evofosfamide [36]. In vivo self-ubiquitination of Ube2E1 is further supported by the high-throughput study aimed to identify all ubiqui
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br In half a century after its first biochemical characteriz
2020-04-07

In 2015–2016, half a century after its first biochemical characterization as a template-independent polymerase, it was shown that TdT can, firstly, assemble a DNA synapsis by itself, optimally with one micro-homology base-pair between strands [] and secondly, perform a template-dependent nucleotid
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br Funding This work was supported by a research grant
2020-04-07

Funding This work was supported by a research grant of the Deutsche Forschungsgemeinschaft (SCHN477-9-2 to R.S.S), the Manfred-Stolte-Stiftung (to R.S.S.) and by a research grant from the German Cancer Aid (Deutsche Krebshilfe, No. 106696/TP 5 to T.F.). Introduction Death-associated protein k
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6-Bnz-cAMP sodium salt synthesis Taken together our results
2020-04-07

Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent som
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Our finding that VEGF A
2020-04-06

Our finding that VEGF-A induced downregulation of EphB4 is VEGFR2 dependent (Fig. 4A) is not surprising because VEGFR2 is the primary signaling receptor of VEGF-A in EC [34]. However, our finding that VEGF-A induced upregulation of dll4 SR 59230A hydrochloride receptor is not inhibited by VEGFR2 in
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In the present study it was particularly
2020-04-06

In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including bungarotoxin pa
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Adenine In all available E E
2020-04-06

In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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